Sunitinib

• Description:

  Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

• Product Name Alternative:

  SU 11248

• UNSPSC:

  12352005

• Hazard Statement:

  H360, H372

• Target:

  Apoptosis; Autophagy; IRE1; Mitophagy; PDGFR; VEGFR

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Autophagy; Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Sunitinib.html

• Purity:

  99.69

• Solubility:

  DMSO : 20.83 mg/mL (ultrasonic)

• Smiles:

  O=C (NCCN (CC) CC) C1=C (NC (/C=C2C (NC3=C\2C=C (C=C3) F) =O) =C1C) C

• Molecular Formula:

  C22H27FN4O2

• Molecular Weight:

  398.47

• Precautions:

  H360, H372

• References & Citations:

  [1]Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol- (3Z) -ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl) amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46 (7) :1116-9.|[2]Ali MM, et al. Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response. EMBO J. 2011 Mar 2;30 (5) :894-905.|[3]O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101 (9) :3597-605.|[4]Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Can

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, protect from light)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  PDGFRβ; VEGFR2/KDR/Flk-1

• Citation 01:

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• CAS Number:

  557795-19-4